HRP20120917T1 - TETRAHIDROCIKLOPENTA[b]INDOLSKI MODULATORI ANDROGENOG RECEPTORA - Google Patents
TETRAHIDROCIKLOPENTA[b]INDOLSKI MODULATORI ANDROGENOG RECEPTORA Download PDFInfo
- Publication number
- HRP20120917T1 HRP20120917T1 HRP20120917AT HRP20120917T HRP20120917T1 HR P20120917 T1 HRP20120917 T1 HR P20120917T1 HR P20120917A T HRP20120917A T HR P20120917AT HR P20120917 T HRP20120917 T HR P20120917T HR P20120917 T1 HRP20120917 T1 HR P20120917T1
- Authority
- HR
- Croatia
- Prior art keywords
- image
- compound
- tetrahydrocyclopenta
- salt according
- cyano
- Prior art date
Links
- IAZKTAKWBHQCGF-UHFFFAOYSA-N 1,2,3,3a-tetrahydrocyclopenta[b]indole Chemical compound N1=C2C=CC=CC2=C2C1CCC2 IAZKTAKWBHQCGF-UHFFFAOYSA-N 0.000 title 1
- 239000000849 selective androgen receptor modulator Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 10
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 2
- -1 [(S)-7-cyano-4-((2R,3S)-3-hydroxy-1-methylpyrrolidine-2- ylmethyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-2-yl]carbamic acid Chemical compound 0.000 claims 2
- 201000001881 impotence Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- FBCDRHDULQYRTB-UHFFFAOYSA-N 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1h-imidazo[5,1-f][1,2,4]triazin-4-one;trihydrate;hydrochloride Chemical compound O.O.O.Cl.CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 FBCDRHDULQYRTB-UHFFFAOYSA-N 0.000 claims 1
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- LKPIGMIUKMRUNF-ZDUSSCGKSA-N [(2S)-7-cyano-4-[(3-fluoro-2-hydroxyphenyl)methyl]-2,3-dihydro-1H-cyclopenta[b]indol-2-yl]carbamic acid Chemical compound C(#N)C1=CC=2C3=C(N(C=2C=C1)CC1=C(C(=CC=C1)F)O)C[C@H](C3)NC(O)=O LKPIGMIUKMRUNF-ZDUSSCGKSA-N 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 230000037182 bone density Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- RIZZCKXDHXXMQI-KRWDZBQOSA-N propan-2-yl n-[(2s)-7-cyano-4-[(5-fluoro-2-hydroxyphenyl)methyl]-2,3-dihydro-1h-cyclopenta[b]indol-2-yl]carbamate Chemical class C([C@H](C1)NC(=O)OC(C)C)C2=C1C1=CC(C#N)=CC=C1N2CC1=CC(F)=CC=C1O RIZZCKXDHXXMQI-KRWDZBQOSA-N 0.000 claims 1
- 229960002639 sildenafil citrate Drugs 0.000 claims 1
- DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 DEIYFTQMQPDXOT-UHFFFAOYSA-N 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229960000835 tadalafil Drugs 0.000 claims 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 229960001540 vardenafil hydrochloride Drugs 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/94—[b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/06—Anabolic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5372208P | 2008-05-16 | 2008-05-16 | |
| PCT/US2009/043875 WO2009140448A1 (en) | 2008-05-16 | 2009-05-14 | Tetrahydrocyclopenta[b]indole androgen receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120917T1 true HRP20120917T1 (hr) | 2012-12-31 |
Family
ID=40847864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120917AT HRP20120917T1 (hr) | 2008-05-16 | 2012-11-13 | TETRAHIDROCIKLOPENTA[b]INDOLSKI MODULATORI ANDROGENOG RECEPTORA |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8486943B2 (sl) |
| EP (1) | EP2297100B1 (sl) |
| JP (1) | JP5603327B2 (sl) |
| KR (1) | KR101278788B1 (sl) |
| CN (1) | CN102026974B (sl) |
| AU (1) | AU2009246348B2 (sl) |
| BR (1) | BRPI0912394A2 (sl) |
| CA (1) | CA2724629C (sl) |
| CY (1) | CY1113341T1 (sl) |
| DK (1) | DK2297100T3 (sl) |
| EA (1) | EA019713B1 (sl) |
| ES (1) | ES2396612T3 (sl) |
| HR (1) | HRP20120917T1 (sl) |
| MX (1) | MX2010012436A (sl) |
| PL (1) | PL2297100T3 (sl) |
| PT (1) | PT2297100E (sl) |
| SI (1) | SI2297100T1 (sl) |
| WO (1) | WO2009140448A1 (sl) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA98777C2 (en) | 2006-11-20 | 2012-06-25 | Эли Лилли Энд Компани | Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators |
| BRPI0907844B8 (pt) | 2008-02-22 | 2021-05-25 | Radius Health Inc | compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos |
| US8268872B2 (en) | 2008-02-22 | 2012-09-18 | Radius Health, Inc. | Selective androgen receptor modulators |
| JP5964756B2 (ja) | 2010-02-04 | 2016-08-03 | ラジウス ヘルス，インコーポレイテッド | 選択的アンドロゲン受容体モジュレーター |
| PL2568806T3 (pl) | 2010-05-12 | 2017-03-31 | Radius Health, Inc. | Schematy lecznicze |
| US8642632B2 (en) | 2010-07-02 | 2014-02-04 | Radius Health, Inc. | Selective androgen receptor modulators |
| WO2012047617A1 (en) | 2010-09-28 | 2012-04-12 | Radius Health, Inc. | Selective androgen receptor modulators |
| FI3122426T3 (fi) | 2014-03-28 | 2023-03-31 | Univ Duke | Rintasyövän hoitaminen käyttäen selektiivisiä estrogeenin reseptorin modulaattoreita |
| US9421264B2 (en) | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| JOP20180072A1 (ar) * | 2014-09-11 | 2019-01-30 | Lilly Co Eli | علاج الأعراض المرتبطة بالعلاج بالحرمان من الأندروجين |
| PL3474841T3 (pl) | 2016-06-22 | 2022-07-11 | Ellipses Pharma Ltd | Sposoby leczenia nowotworu złośliwego piersi ar+ |
| US20180185347A1 (en) * | 2016-11-16 | 2018-07-05 | Transition Therapeutics (Ireland 2) Limited | Tetrahydrocyclopenta[b]indole compounds and phosphodiesterase inhibitors for the treatment of the signs and symptoms of bhp |
| AU2018205285C9 (en) | 2017-01-05 | 2024-05-23 | Radius Pharmaceuticals, Inc. | Polymorphic forms of RAD1901-2HCl |
| CA3104395A1 (en) | 2018-07-04 | 2020-01-09 | Radius Pharmaceuticals, Inc. | Polymorphic forms of rad1901-2hcl |
| WO2022010951A1 (en) * | 2020-07-06 | 2022-01-13 | Crescenta Biosciences | Antiviral use of fabp4 modulating compounds |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4988820A (en) | 1986-02-21 | 1991-01-29 | Bayer Aktiengesellschaft | Cycloalkano(1,2-B) indole-sulponamides |
| GB8924392D0 (en) | 1989-10-30 | 1989-12-20 | Bayer Ag | Substituted cycloalkano/b/dihydroindole-and-indolesulphonamides |
| GB9008108D0 (en) | 1990-04-10 | 1990-06-06 | Bayer Ag | Cycloalkano(b)dihydroindoles and-indolesulphonamides substituted by heterocycles |
| DE4027278A1 (de) | 1990-08-29 | 1992-03-05 | Bayer Ag | Heterocyclisch substituierte indolsulfonamide |
| DE4131346A1 (de) | 1991-09-20 | 1993-03-25 | Bayer Ag | Indolsulfonamid substituierte dihydropyridine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln |
| JP2005527464A (ja) | 2001-08-09 | 2005-09-15 | イーライ・リリー・アンド・カンパニー | ｓＰＬＡ２インヒビターとしてのシクロヘプタＢインドール誘導体 |
| DE10164564B4 (de) | 2001-12-14 | 2007-05-16 | Zentaris Gmbh | Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR) |
| AU2003231509A1 (en) | 2002-05-16 | 2003-12-02 | Shionogi And Co., Ltd. | Compound exhibiting pgd 2 receptor antagonism |
| US20060074124A1 (en) | 2003-09-12 | 2006-04-06 | Andrew Napper | Methods of treating a disorder |
| US7019022B2 (en) | 2003-12-15 | 2006-03-28 | Merck Frosst Canada & Co. | Substituted tetrahydrocarbazole and cyclopentanoindole derivatives |
| CN1926104A (zh) | 2004-03-03 | 2007-03-07 | 伊莱利利公司 | 作为类固醇激素核受体调节剂的双环取代的吲哚衍生物 |
| WO2006058088A2 (en) | 2004-11-23 | 2006-06-01 | Ptc Therapeutics, Inc. | Carbazole, carboline and indole derivatives useful in the inhibition of vegf production |
| BRPI0608353A2 (pt) * | 2005-02-17 | 2009-12-01 | Wyeth Corp | derivados de indol, benzotiofeno, benzofurano e indeno cicloalquilfundidos |
| AU2006262283B2 (en) * | 2005-06-24 | 2011-10-13 | Eli Lilly And Company | Tetrahydrocarbazole derivatives useful as androgen receptor modulators (SARM) |
| WO2007047604A2 (en) | 2005-10-18 | 2007-04-26 | Elixir Pharmaceuticals, Inc. | Sirt1 inhibition |
| WO2008019825A1 (en) | 2006-08-14 | 2008-02-21 | Santhera Pharmaceuticals (Schweiz) Ag | Use of tricyclic indole derivatives for the treatment of muscular diseases |
| UA98777C2 (en) * | 2006-11-20 | 2012-06-25 | Эли Лилли Энд Компани | Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators |
-
2009
- 2009-05-14 PT PT97475313T patent/PT2297100E/pt unknown
- 2009-05-14 PL PL09747531T patent/PL2297100T3/pl unknown
- 2009-05-14 MX MX2010012436A patent/MX2010012436A/es active IP Right Grant
- 2009-05-14 KR KR1020107025588A patent/KR101278788B1/ko active IP Right Grant
- 2009-05-14 US US12/989,959 patent/US8486943B2/en active Active
- 2009-05-14 ES ES09747531T patent/ES2396612T3/es active Active
- 2009-05-14 DK DK09747531.3T patent/DK2297100T3/da active
- 2009-05-14 EA EA201071317A patent/EA019713B1/ru not_active IP Right Cessation
- 2009-05-14 WO PCT/US2009/043875 patent/WO2009140448A1/en active Application Filing
- 2009-05-14 JP JP2011509679A patent/JP5603327B2/ja active Active
- 2009-05-14 SI SI200930447T patent/SI2297100T1/sl unknown
- 2009-05-14 AU AU2009246348A patent/AU2009246348B2/en not_active Ceased
- 2009-05-14 CA CA2724629A patent/CA2724629C/en not_active Expired - Fee Related
- 2009-05-14 CN CN200980117076XA patent/CN102026974B/zh active Active
- 2009-05-14 EP EP09747531A patent/EP2297100B1/en active Active
- 2009-05-14 BR BRPI0912394A patent/BRPI0912394A2/pt not_active IP Right Cessation
-
2012
- 2012-11-13 HR HRP20120917AT patent/HRP20120917T1/hr unknown
- 2012-11-14 CY CY20121101095T patent/CY1113341T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102026974B (zh) | 2013-08-28 |
| US20110039855A1 (en) | 2011-02-17 |
| EA019713B1 (ru) | 2014-05-30 |
| EP2297100B1 (en) | 2012-10-31 |
| CN102026974A (zh) | 2011-04-20 |
| EA201071317A1 (ru) | 2011-06-30 |
| CA2724629A1 (en) | 2009-11-19 |
| BRPI0912394A2 (pt) | 2016-07-26 |
| JP2011520903A (ja) | 2011-07-21 |
| KR20100132551A (ko) | 2010-12-17 |
| US8486943B2 (en) | 2013-07-16 |
| AU2009246348A8 (en) | 2010-12-16 |
| MX2010012436A (es) | 2010-12-06 |
| CA2724629C (en) | 2014-08-19 |
| PT2297100E (pt) | 2013-01-24 |
| WO2009140448A8 (en) | 2010-01-07 |
| SI2297100T1 (sl) | 2013-02-28 |
| AU2009246348B2 (en) | 2012-04-12 |
| JP5603327B2 (ja) | 2014-10-08 |
| AU2009246348A1 (en) | 2009-11-19 |
| CY1113341T1 (el) | 2016-06-22 |
| ES2396612T3 (es) | 2013-02-22 |
| EP2297100A1 (en) | 2011-03-23 |
| WO2009140448A1 (en) | 2009-11-19 |
| KR101278788B1 (ko) | 2013-06-25 |
| DK2297100T3 (da) | 2012-12-17 |
| PL2297100T3 (pl) | 2013-03-29 |
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